1. Field of the Invention
The present invention relates to compositions of matter classified in the art of chemistry as .alpha.-(aminoalkyl)-4-hydroxy-3-(alkylthio)benzenemethanols and to a method of using the same for reducing blood pressure in mammals.
2. Information Disclosure Statement
Philion U.S. Pat. No. 4,374,149, issued Feb. 15, 1983 and pending Philion application Ser. No. 937,927, filed Aug. 30, 1978, disclose respective .alpha.-(aminoalkyl)-4-hydroxy-3-(alkylsulfinyl)benzenemethanols and .alpha.-(aminoalkyl)-4-hydroxy-3-(alkylsulfonyl)benzenemethanols.
Buu-Hoi et al. U.S. Pat. No. 3,954,871 issued May 4, 1976 (corresponds to Continental Pharma British Specification No. 1,321,701, published June 27, 1973, referred to in parent application Ser. No. 937,926) discloses a group of compounds embraced by the generic formula ##STR1## wherein, inter alia: R.sub.1 is RS, RSO or RSO.sub.2 (R=H, or C.sub.1 -C.sub.10 alkyl);
R.sub.2 and R.sub.3 are hydrogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; PA1 R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; and PA1 R.sub.5 and R.sub.6 are independently hydrogen or C.sub.1 -C.sub.16 alkyl optionally substituted by a phenyl or substituted phenyl group. PA1 n is an integer from 1 to 3; PA1 Ar is phenyl or phenyl having from one to three substituents selected from the group consisting of halo, lower alkyl, hydroxy and lower alkoxy; PA1 R is lower alkyl; PA1 Y is hydrogen, lower alkanoyl, aroyl, benzenesulfonyl or toluenesulfonyl;
The compounds are stated to exhibit .beta.-adrenergic blocking, peripheral vasodilator, antiarrhythmic and hypotensive activities.
Lutz, et al., J. Med. Chem. 15, 795-802 (1972), disclose the attempted preparation of 4-hydroxy-3-mercaptophenylethanolamine, i.e.: ##STR2## The compound however was neither isolated as a single entity nor characterized. Also disclosed is 4-hydroxy-3-mercaptophenylethylamine.
Pratesi, et al. British Specification No. 1,154,193, published June 4, 1969 discloses as a .beta.-adrenergic agent .alpha.-[(isopropylamino)methyl]-3-(methylthio)benzenemethanol, i.e.: ##STR3##
In the field of antihypertensive therapy the use of peripheral vasodilator agents to lower blood pressure has often suffered a serious disadvantage, namely, the reflex tachycardia elicited by the hypotension induced by systemic vasodilation. Recently efforts have been made to overcome this problem by employing hypotensive vasodilators in combination with .beta.-adrenergic blocking agents, the function of the latter being to reduce the reflex tachycardia caused by the vasodilator-induced hypotension. This mode of therapy of course suffers the inconvenience of requiring two separate drugs and the attendant need for separate dosage regulation as well as the increased potential for patient error in failing to administer either one or the other of the drugs.